Pharmaceutical and cosmetic composition against skin aging

ABSTRACT

Pharmaceutical and cosmetic compositions for the prevention of skin aging, containing phospholipid complexes of extracts of  Vitis vinifera , and phospholipid complexes of standardized extract from  Centella asiatica.

FIELD OF THE INVENTION

The present invention relates to pharmaceutical and cosmeticcompositions against the skin aging containing ingredients of vegetableorigin.

More particularly, the present invention relates to pharmaceutical andcosmetic compositions for the prevention of skin aging, containingphospholipid complexes of extracts of Vitis vinifera, and phospholipidcomplexes of triterpenes extracted from Centella asiatica.

BACKGROUND OF THE INVENTION

Skin aging is a complex biological process affecting various layers ofthe skin, but whose major effects are seen in the dermis. There are twobiologically independent aging processes that occur simultaneously. Thefirst is intrinsic aging, which affects skin as well as, most likely,the internal organs. The second is extrinsic aging or photo-aging whichis the result of exposure to the elements, primarily ultravioletirradiation. The consequences of innate aging can be observed all overthe skin, including areas protected from the sun. In the areas exposedto the sun, particularly the face and the backs of the hands, photoagingdamage is superimposed to tissue degeneration due to innate aging. Thus,the most noticeable changes on facial and neck skin, the primary areasthat patients are concerned about, result from the combination ofintrinsic and extrinsic aging processes. It has been suggested that asmuch as 80% of facial aging may be ascribed to exposure to the sun,although other factors (i.e. cigarette smoking) can contribute topremature wrinkling.

From a biochemical standpoint, photoaging is thought to be inducedmainly by: some proteases, mainly metalloproteases, which areoverproduced and overrealesed by keratinocytes and fibroblasts as aconsequence of the interaction with ultraviolet radiation (theseproteases are degradative enzymes irreversibly damaging collagen,elastin and hyaluronic acid, bringing about dermis scars and visiblewrinkles); and by oxidative stress, able to eliminate the normal skinantioxidant defenses in a very short time.

OBJECT OF THE INVENTION

On the basis of these general considerations, it is clear the need toprotect the skin from premature aging by a tool able to counteract theaction of the proteases on the dermis (while increasing the capabilityof fibroblasts to produce and release new collagen fibers) and thedisappearance of the antioxidant defenses from the skin.

SUMMARY OF THE INVENTION

The present invention fulfills this need to protect the skin frompremature aging, by providing pharmaceutical and cosmetic compositionscontaining the following ingredients of vegetable origin:

-   a) phospholipid complexes of standardized extract 0.1-2.5% of Vitis    vinifera,-   b) phospholipid complexes of standardized extract 0.1-2.5% of    Centella asiatica.

More preferably, the pharmaceutical and cosmetic compositions of thepresent invention contain the following ingredients of vegetable originin the following percentages:

-   a) phospholipid complexes of standardized extract 1% of Vitis    vinifera,-   b) phospholipid complexes of standardized extract 1% of Centella    asiatica.

The phospholipid complexes of standardized extract of Vitis vinifera(also referred to as “components a”) are disclosed in EP 275,224. Saidextracts consist of the polyphenolic fraction contained in Vitisvinifera seeds, and comprise gallic acid, monomers, dimers, trimers,tetramers, pentamers, examers and heptameters of catechin andepicatechin free and esterified with gallic acid.

In vitro and in vivo studies have evidenced the high antioxidizingactivity of said extracts (10 to 200 times as much that of vitamin E,depending on the experimental model), which includes the scavenging ofthe most reactive radical species, and counteracts all the phenomenarelated to the activity of free radicals. Said extract is furthercharacterized by the capability to inhibit xanthine-oxidase and tochelate Cu++ and Fe+++, thus preventing the enzymatic release of freeradicals in tissues. Finally, the extract of Vitis vinifera inhibitscollagenase and other proteases, thereby protecting the connectivetissue and the skin from the harmful action of proteolytic enzymesreleased following UV irradiation and during the development of aninflammatory skin response, and it has selective affinity to the skinand the circulatory structures, such as microvessels and capillaries,thereby also protecting the microcirculatory district.

The phospholipid complexes of standardized extract of Centella asiatica(also referred to as “components b”) are disclosed in EP 283,713.

This extract consists of a 4:3:3 mixture of three different moleculeshaving strong activity on collagen metabolism: asiaticoside, asiaticacid and madecassic acid. These molecules improve the capability of thefibroblasts to up-take amino acids such as L-Proline andL-Hydroxyproline that, from a quali-quantitative standpoint, are themost important amino acids in the collagen formula. An improvedsynthesis of collagen means a faster substitution of the degraded oldfibers of collagen with the new ones.

Components a) and b), when tested toxicologically, showed. neither toxicnor irritative actions towards the treated tissues.

The compositions of the present invention may optionally contain, inaddition to components a) and b) indicated above, also other activeingredients such as vitamin E (0.2-1%), zinc (0.1-0.3%), hydroxyacids(0.1-1%) and glycyrrhetinic acid or a complex thereof with phospholipids(0.1-2.5%), to improve the antioxidant, anti-aging and antinflammatoryproperties of the composition.

The compositions of the present invention will be administeredtopically, in the form of suitable formulations liquid (such as gel,lotions, milks, emulsions, foams and the like) or solid or semi-solid(such as creams, ointments, lipsticks, and the like). Said formulationswill be prepared according to conventional methods, such as thosedescribed in “Remington's Pharmaceutical Handbook”, Mack Publishing Co.,NY, USA, together with suitable excipients, such as emollients,moisturizers, thickening agents, emulsifiers, dyes, flavors and thelike.

Some examples of compositions according to the invention are reported inthe following.

EXAMPLE 1 Oil-in-Water Emulsion

100 g contain: Phospholipid complexes of extract of Vitis vinifera 0.20g Phospholipid complexes of triterpenes extracted from 1.00 g Centellaasiatica Isostearyl isostearate (Gattefossé) 2.50 g Polyisoprene(Syntesqual - Vevy) 2.50 g Decyl oleate (Cetiol V - Henkel) 2.00 g Cetylpalmitate (Cutina CP - Henkel) 2.00 g Cetearyl Isononanoate (Cetiol SN -Henkel) 2.00 g Polysorbate 80 (Tween 80 - ICI) 1.00 g Imidazolidinylurea 0.30 g Tocoferol 0.20 g Ascorbyl Palmitate 0.10 g Methylchloroisothiazolinone (e) Methyl isothiazolinone (Kathon CG-Rohm & Haas)0.05 g Disodium EDTA 0.10 g Butylated hydroxytoluene 0.05 gPolyacrylamide (e) C₁₃₋₁₄ Isoparaffin (e) Laureth-7 (Spiegel 305 -Seppic) 2.50 g Perfume 0.10 g Purified water q.s. to 100.0 g 

EXAMPLE 2 Oil-in-Water Emulsion

100 g contain: Phospholipid complexes of extract of Vitis vinifera 0.50g Phospholipid complexes of triterpenes extracted from 0.50 g Centellaasiatica Phospholipid complexes of glycyrrhetinic acid 1.50 g C₁₂₋₁₅Alkyl benzoate (Finsolv TN - Finetex) 4.00 g Cetyl palmitate (CutinaCP - Henkel) 3.00 g Polyisoprene (Syntesqual - Vevy) 2.50 g Isostearylisostearate (Gaffefossé) 2.50 g Polysorbate 80 (Tween 80 - ICI) 1.00 gImidazolidinyl urea 0.30 g Methyl chloroisothiazolinone (e) Methylisothiazolinone (Kathon CG-Rohm & Haas) 0.05 g Tocoferol 0.20 g AscorbylPalmitate 0.10 g Disodium EDTA 0.10 g Citric acid 0.05 g Polyacrylamide(e) C₁₃₋₁₄ Isoparaffin (e) 2.00 g Laureth-7 (Spiegel 305 - Seppic)Butylated hydroxytoluene 0.05 g Perfume 0.10 g Purified water q.s. to100.0 g 

1. A composition comprising: phospholipid complexes of standardizedextract of Vitis vinifera; and phospholipid complexes of standardizedextract of Centella asiatica and wherein said extracts are of vegetableorigin.
 2. The composition according to claim 1, further comprising atleast one additional active ingredient selected from the groupconsisting of vitamin E, zinc, hydroxyacids, glycyrrhetinic acid and acomplex of glycyrrhetinic acid with phospholipids.
 3. The compositionaccording to claim 1, further comprising at least one carrier orexcipient selected from the group consisting of emollients,moisturizers, thickening agents, emulsifiers, dyes, and flavors.
 4. Thecomposition according to claim 1, wherein said composition is a cosmeticcomposition for retarding noticeable effects of skin aging.
 5. Thecomposition according to claim 1, wherein said phospholipid complexes ofstandardized extract of Vitis vinifera are present in an amount of0.1-2.5% of said composition, and said phospholipid complexes ofstandardized extract of Centella asiatica are present in an amount of0.1-2.5% of said composition.
 6. A composition comprising: 0.1-2.5%phospholipid complexes of standardized extract of Vitis vinifera;0.1-2.5% phospholipid complexes of standardized Extract of Centellaasiatica; a carrier or an excipient, wherein said extracts are ofvegetable origin, and said composition does not contain fish cartilageextract.
 7. The composition of claim 6, wherein said carrier orexcipient is selected from the group consisting of emollients,moisturizers, thickening agents, emulsifiers, dyes, flavors and mixturesthereof.
 8. The composition according to claim 6, further comprising atleast one additional active ingredient selected from the groupconsisting of vitamin E, zinc, hydroxyacids and glycyrrhetinic acid anda complex of glycyrrhetinic acid with phospholipids.
 9. The compositionaccording to claim 6, wherein said composition is a cosmetic compositionfor retarding skin aging.
 10. A composition comprising: 0.1-2.5%phospholipid complexes of standardized extract of Vitis vinifera;0.1-2.5% phospholipid complexes of standardized Extract of Centellaasiatica; at least one of a pharmaceutically acceptable carrier and apharmaceutically acceptable excipient and wherein said extracts are ofvegetable origin.